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GLASS

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Go to the GPCR, ligand, or experimental data tables.
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GPCR

Name	Glucose-dependent insulinotropic receptor
Species	Homo sapiens (Human)
Gene	GPR119
Synonym	GPCR2 GPR119 G-protein coupled receptor 2 G-protein coupled receptor 119 G protein-coupled receptor 119 glucose-dependent insulinotropic receptor [ Show all ]
Disease	Type 2 diabetes Diabetes Peripheral arterial disease; Type 2 diabetes Non-insulin dependent diabetes Gastric cancer; Type 2 diabetes
Length	335
Amino acid sequence	MESSFSFGVILAVLASLIIATNTLVAVAVLLLIHKNDGVSLCFTLNLAVADTLIGVAISGLLTDQLSSPSRPTQKTLCSLRMAFVTSSAAASVLTVMLITFDRYLAIKQPFRYLKIMSGFVAGACIAGLWLVSYLIGFLPLGIPMFQQTAYKGQCSFFAVFHPHFVLTLSCVGFFPAMLLFVFFYCDMLKIASMHSQQIRKMEHAGAMAGGYRSPRTPSDFKALRTVSVLIGSFALSWTPFLITGIVQVACQECHLYLVLERYLWLLGVGNSLLNPLIYAYWQKEVRLQLYHMALGVKKVLTSFLLFLSARNCGPERPRESSCHIVTISSSEFDG
UniProt	Q8TDV5
Protein Data Bank	N/A
GPCR-HGmod model	Q8TDV5
3D structure model	This predicted structure model is from GPCR-EXP Q8TDV5.
BioLiP	N/A
Therapeutic Target Database	T93788
ChEMBL	CHEMBL5652
IUPHAR	126
DrugBank	N/A

Ligand

Name	CHEMBL2312505
Molecular formula	C25H31N5O3
IUPAC name	(1-methylcyclopropyl) 6-[5-ethyl-6-(2-methylpyridin-3-yl)oxypyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylate
Molecular weight	449.555
Hydrogen bond acceptor	7
Hydrogen bond donor	0
XlogP	4.3
Synonyms	BDBM50424563
Inchi Key	AZDUDBIUEWKFGT-UHFFFAOYSA-N
Inchi ID	InChI=1S/C25H31N5O3/c1-4-20-22(27-14-28-23(20)32-21-6-5-9-26-15(21)2)29-16-10-18-12-17(29)13-19(11-16)30(18)24(31)33-25(3)7-8-25/h5-6,9,14,16-19H,4,7-8,10-13H2,1-3H3
PubChem CID	71546035
ChEMBL	CHEMBL2312505
IUPHAR	N/A
BindingDB	50424563
DrugBank	N/A
Structure SDF download
Lipinski's druglikeness	This ligand satisfies Lipinski's rule of five.

Experimental Data

Parameter	Value	Reference	Database source
EC50	49.0 nM	PMID23234271	BindingDB,ChEMBL
Intrinsic activity	52.0 %	PMID23234271	ChEMBL
Ki	123.0 nM	PMID23234271	BindingDB,ChEMBL

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